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Assay Detail

CHEMBL4189690

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of recombinant human BLK using Poly(Glu, Tyr) 4:1 as substrate after 1 hr by ELISA
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Tyrosine-protein kinase Blk (CHEMBL2250)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of 4,7-Diamino-5-(4-phenoxyphenyl)-6-methylene-pyrimido[5,4- b]pyrrolizines as Novel Bruton's Tyrosine Kinase Inhibitors.
Xue Y, Song P, Song Z, Wang A, Tong L, Geng M, Ding J, Liu Q, Sun L, Xie H, Zhang A.
J Med Chem (2018) 61 : 4608 -4627
PubMed 29715023 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 9.50 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4211949 1 9.70
CHEMBL1873475 IBRUTINIB 4.0 1 9.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4211949 IC50 = 0.2 nM 9.70
CHEMBL1873475 IBRUTINIB IC50 = 0.5 nM 9.30